JPH0481962B2 - - Google Patents

Description

[Detailed description of the invention]

[Industrial Field of Application] The present invention relates to a skin preparation for external use that has an excellent anti-inflammatory effect and is made by blending a specific hydroquinone glycoside with glycyrrhetin and/or its glycoside. [Prior Art] Glymethylretin, also called glymethylretinoic acid, is a compound structurally similar to steroid hormones. Glycyrrhetin has been proven to have anti-inflammatory effects in animal and clinical experiments, and is used for anti-inflammatory purposes, eczema, etc.
It is often added to cosmetics and pharmaceuticals to treat dermatitis, measles, and drug eruptions. It is also said to have a hair growth effect, and is sometimes included in hair tonics. Furthermore, as a glycoside of glycyrrhetin, glycyrrhizin, which is formed by conjugating two molecules of glucuronic acid to glycyrrhetin, is a typical example, and this is also known to have similar effects. . [Problems to be Solved by the Invention] The present inventors have been conducting research on the medicinal efficacy of glycyrrhetin and its glycosides for many years, and have surprisingly discovered that the combination use of a specific hydroquinone glycoside has been found to synergistically enhance the medicinal efficacy of glycyrrhetin or its glycosides.
The present invention is based on this knowledge. [Means for solving the problems] That is, the present invention provides glycyl methylene and/or
or a glycoside thereof and hydroquinone-β-D-glucoside (arbutin). Hereinafter, the configuration of the present invention will be explained in detail. In the present invention, glycyrrhetin and/or its glycosides are blended into the skin external preparation base. Glycyrrhizin is well known as a glycoside. The blending amount is within the range of 0.1 to 5% by weight of the total amount of the skin external preparation; if it is less than 0.1% by weight, the medicinal efficacy of glycyrrhizin cannot be expected, and even if it is blended in more than 5% by weight, the effect will be further increased. is small and uneconomical. It is known that glycyrrhizin is also present in licorice as a sweet component, but in the present invention, it is of course possible to incorporate it as a licorice extract. In the present invention, the hydroquinone glycoside that is incorporated into the skin external preparation together with glycyrrhetin and/or its glycoside to synergistically enhance the medicinal efficacy of glycyrrhetin and/or its glycoside is represented by the following general formula (). Ru. {In formula (), R represents a pentose residue, a hexose residue, an amino sugar residue, a uronic acid residue, or a methylated product thereof. } In formula (), R is L-arabinose, D-arabinose, D-xylose, D-ribose, L
- Residues of pentose sugars such as xylulose, L-lyxose, D-ribulose, D-glucose, D-galactose, L-galactose, D-mannose, D-talose, D-fructose, L-sorbose, D-tagatose , residues of hexose sugars such as D-psicose, residues of amino sugars such as D-glucosamine, D-galactosamine, sialic acid, aminouronic acid, muramic acid, D-glucuronic acid, D-
Residues of uronic acids such as galacturonic acid, D-mannuronic acid, L-iduronic acid, and L-guluronic acid, or methylated products thereof. Among these, R is a residue of D-glucose;
Particularly preferred is hydroquinone with D-glucose β-bonded, that is, hydroquinone-β-D-glucose (common name: arbutin). The amount of arbutin in the total amount of the skin external preparation is
0.1-30% by weight, preferably 6-20% by weight. The skin external preparation in which glycyrrhetin and/or its glycoside and arbutin should be blended may be a conventional skin external preparation, such as an aqueous solution system, a solubilized system, an emulsion system, a powder dispersion system, a water-oil two-layer system, or a water-oil system. -Oil-Powder 3
Any type of base may be used, including layered bases, and can be used for basic cosmetics such as lotions, emulsions, creams, and packs.
In addition to cosmetics such as makeup cosmetics such as lipsticks and foundations, and hair cosmetics such as shampoos, conditioners, and hair tonics, our products range from pharmaceuticals to quasi-drugs. The skin external preparation of the present invention may contain oil, a humectant, a thickener, a preservative, an emulsifier, an anti-emulsifying agent, a sequestering agent, an ultraviolet absorber, and the like, as necessary, within a range that does not impair the effects of the present invention. Powders, drugs, colorants, fragrances, etc. can be added. [Example] Next, the present invention will be explained in further detail with reference to Examples and Comparative Examples. The present invention is not limited to these. The blending amount is in weight%. Examples 1 to 3, Comparative Examples 1 to 3 Using the following lotion as a base, Examples and Comparative Examples were prepared in which glycyrrhetin and arbutin shown in Table 1 were blended, respectively. (Base) Ethanol 3.0 1,3-butylene glycol 10.0 POE (polyoxyethylene, same below, 15 mol)
Oleyl ether 0.5 Oleyl alcohol 01 Ethylparaben 0.1 Fragrance 0.05 Purified water Residual

[Table] Examples 1 to 3 and Comparative Examples 1 to 2 were subjected to actual use tests to evaluate their anti-inflammatory effects in suppressing hot flashes on the skin after sunburn. The test method is as follows. (Test method) Six groups of 15 women in their 20s to 30s were used as subjects, and after swimming at the beach for half a day in summer, each group was given two doses of either Examples 1 to 3 or Comparative Examples 1 to 2 as appropriate. After using the product for several days, we asked them how satisfied they were with the anti-inflammatory effect. The results are shown in Table-2. The numbers in Table 2 are the number of people out of 15 who answered that they were satisfied. It is clear that arbutin has the effect of further increasing the anti-inflammatory effect of glycyrrhizin.

[Table] Example 4 Night cream A Setanol 4.0 Vaseline 7.0 Squalane 21.0 Stearic acid monoglyceride 2.2 POE(20) sorbitan monostearate 2.8 Isopropyl myristate 6.0 Ethylparaben 0.3 Fragrance 0.2 B Propylene glycol 10.0 1,3-butylene glycol 5.0 Glycyrrhizin 0.1 Arbutin 2.0 Purified water Residue (manufacturing method) The oil phase component belonging to A and the aqueous phase component belonging to B are separately heated and dissolved, and the oil phase is mixed into the water phase to emulsify. , and cooled to room temperature to obtain cream. Example 5 Water-absorbing ointment vaseline 40.0 Stearyl alcohol 15.0 Mokuro 15.0 POE(10) oleate 0.25 Stearic acid monoglyceride 0.25 Glycyrrhizin 3.0 Arbutin 3.0 Purified water Residue (manufacturing method) According to Example 4. Example 6 Hair tonic ethanol 50.0 POE(8) oleyl ether 1.5 Hinoxathiol 0.1 Glycyrrhizin 1.0 Arbutin 1.0 Ethylparaben 0.1 Fragrance 0.05 Purified water Remaining (manufacturing method) POE oleyl ether in part of the ethanol,
Dissolve hinokitiol, ethylparaben and fragrance. Separately, glycyrrhizin and arbutin were dissolved in the remaining purified water and ethanol, and the ethanol phase was added to obtain hair tonic. Examples 4 to 6 all had excellent anti-inflammatory effects, and were also excellent in stability over time, usability, and stability. [Effects of the Invention] According to the present invention, an external skin preparation containing glycyrrhizin and a hydroquinone glycoside is an external skin preparation that synergistically enhances the medicinal efficacy of glycyrrhizin.

Claims (1)

[Claims] 1. A skin external preparation characterized by containing glycyrrhetin and/or its glycoside and hydroquinone-β-D-glucoside.